龙源期刊网 https://www.doczj.com/doc/185792130.html,
载姜黄素介孔二氧化硅纳米粒的制备及其体外抗肿瘤活性研究
作者：何黎黎顾健
来源：《中国中药杂志》2015年第21期
[摘要] 制备载姜黄素（curumin，Cur）的介孔二氧化硅纳米粒（mesoporous silica nanoparticles，MSN），考察其体外释药行为和抗肿瘤活性。采用聚合法制备了MSN，并运用溶剂挥干法和浸渍离心法制备了载Cur的MSN（Cur-MSN），以包封率和载药量为指标优化了制备工艺。通过扫描电镜表征了Cur-MSN形态，测定了Cur-MSN粒径大小和电位。以
0.2% SDS溶液为释放介质，研究了Cur-MSN的体外释放行为，并考察了Cur-MSN对HeLa细胞的杀伤作用。运用优化工艺制备的Cur-MSN圆整均一，具有典型的介孔结构特征，平均粒径为75.8 nm，Zeta电位为-30.1 mV；3批Cur-MSN的平均包封率为（72.55±2.01）%，载药量为（16.21±1.12）%。Cur-MSN体外释药行为明显了缓释特征，96 h释放了83.5%；Cur-MSN 对HeLa细胞的杀伤作用呈现浓度依赖性，IC50为19.40 mg·L-1，与Cur的杀伤作用相似。
[关键词] 姜黄素；介孔二氧化硅纳米粒；体外释药；抗肿瘤活性
[Abstract] This paper is to prepare curcumin （Cur） loaded mesoporous silica nanoparticle （Cur-MSN）， evaluate its release behavior and anti-cancer activity in vitro. Mesoporous silica nanoparticle （MSN） was prepared by polymerization method and Cur-MSN was obtained using solvent evaporation method and impregnation centrifugation method. The preparation method was optimized using entrapment efficiency （EE） and loading efficiency （LE） as indexes. Cur-MSN was characterized with scanning electron microscope and its particle size and zeta potential were determined. Finally， in vitro release behavior in 0.2% SDS solution and its cell-killing effect on HeLa cells were also evaluated. The Cur-MSN prepared with process optimization method was round and uniform and exhibited typical mesoporous characterization. The mean particle size and Zeta potential of Cur-MSN were 75.8 nm and -30.1 mV， respectively. EE and LE of three batches of Cur-MSN were （72.55±2.01）% and （16.21±1.12）%， respectively. In vitro release behavior of Cur-MSN showed a sustained release profile with 83.5% cumulative release within 96 h. The killing effect of Cur-MSN on HeLa cells was dose-dependent with IC50 of 19.40 mg·L-1， which was similar to that of Cur.
[Key words] curumin（Cur）； mesoporous silica nanoparticle （MSN）； in vitro release；anti-cancer activity
doi：10.4268/cjcmm20152113
姜黄素（curumin，Cur）是从多年生草本植物姜黄的根茎中提取出来的多酚类化合物，具有多方面的药理作用，尤其可作为一种具有良好应用前景的抗癌药物 [1-2]。但由于姜黄素水